Mofegiline

Mofegiline
Systematic (IUPAC) name
(2E)-2-(fluoromethylidene)-4-(4-fluorophenyl)butan-1-amine
Clinical data
Routes of
administration		 Oral[1]
Legal status
  • Development terminated
Pharmacokinetic data
Biological half-life 1–3 hours[1]
Excretion Urine[2]
Identifiers
CAS Number 119386-96-8
ATC code None
PubChem CID 6437850
ChemSpider 4942371
UNII 1FMJ6D8Y1B
Synonyms MDL-72,974A
Chemical data
Formula C11H13F2N
Molar mass 197.224 g/mol

Mofegiline (MDL-72,974) is a selective, irreversible inhibitor of monoamine oxidase B (MAO-B) and semicarbazide-sensitive amine oxidase (SSAO) which was under investigation for the treatment of Parkinson's disease and Alzheimer's disease,[3][4][5][6] but was never marketed.[7]

Synthesis

Mofegiline synthesis:[8][9]

See also

References

  1. 1 2 Stoltz M, Reynolds D, Elkins L, Salazar D, Weir S (September 1995). "Pharmacokinetics and pharmacodynamics of the monoamine oxidase B inhibitor mofegiline assessed during a phase I dose tolerance trial". Clinical Pharmacology and Therapeutics 58 (3): 342–53. doi:10.1016/0009-9236(95)90252-X. PMID 7554709.
  2. ↑ Dulery BD, Schoun J, Zreika M, et al. (March 1993). "Pharmacokinetics of and monoamine oxidase B inhibition by (E)-4-fluoro-beta-fluoromethylene benzene butanamine in man". Arzneimittel-Forschung 43 (3): 297–302. PMID 8489556.
  3. ↑ Palfreyman MG, McDonald IA, Bey P, Schechter PJ, Sjoerdsma A (1988). "Design and early clinical evaluation of selective inhibitors of monoamine oxidase". Progress in Neuro-psychopharmacology & Biological Psychiatry 12 (6): 967–87. doi:10.1016/0278-5846(88)90092-9. PMID 3266532.
  4. ↑ Zreika M, Fozard JR, Dudley MW, Bey P, McDonald IA, Palfreyman MG (1989). "MDL 72,974: a potent and selective enzyme-activated irreversible inhibitor of monoamine oxidase type B with potential for use in Parkinson's disease". Journal of Neural Transmission. Parkinson's Disease and Dementia Section 1 (4): 243–54. doi:10.1007/bf02263478. PMID 2597310.
  5. ↑ Palfreyman MG, McDonald IA, Bey P, Danzin C, Zreika M, Cremer G (1994). "Haloallylamine inhibitors of MAO and SSAO and their therapeutic potential". Journal of Neural Transmission. Supplementum 41: 407–14. doi:10.1007/978-3-7091-9324-2_54. ISBN 978-3-211-82521-1. PMID 7931257.
  6. ↑ Thiffault C, Quirion R, Poirier J (March 1998). "Effect of the MAO-B inhibitor, MDL72974, on superoxide dismutase activity and lipid peroxidation levels in the mouse brain". Synapse 28 (3): 208–11. doi:10.1002/(SICI)1098-2396(199803)28:3<208::AID-SYN3>3.0.CO;2-E. PMID 9488505.
  7. ↑ Ganellin, C. R.; Triggle, D. J.; Macdonald, F. (1997). Dictionary of pharmacological agents. CRC Press. p. 1370. ISBN 978-0-412-46630-4. Retrieved 25 November 2011.
  8. ↑ McDonald, Ian A.; Lacoste, Jean Michel; Bey, Philippe; Palfreyman, Michael G.; Zreika, Monique (1985). "Enzyme-activated irreversible inhibitors of monoamine oxidase: Phenylallylamine structure-activity relationships". Journal of Medicinal Chemistry 28 (2): 186. doi:10.1021/jm00380a007. PMID 3968682.
  9. ↑ I. A. McDonald, M. G. Palfreyman, EP 295604 (1988 to Merrell Dow).
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